182541
Aromatase Inhibitor II, Letrozole
The Aromatase Inhibitor II, Letrozole, also referenced under CAS 112809-51-5, controls the biological activity of Aromatase.
别名:
Aromatase Inhibitor II, Letrozole, 4,4ʹ-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile, 1-( bis-(4-Cyanophenyl)methyl)-1,2,4-triazole
InChI
1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H
InChI key
HPJKCIUCZWXJDR-UHFFFAOYSA-N
assay
≥99% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
ethanol: <5 mg/mL (partially soluble), DMSO: 50 mg/mL, clear, colorless
shipped in
ambient
Quality Level
General description
An orally bioavailable non-steroidal triazole compound that acts as a potent and selective inhibitor of aromatase (IC50 = 140, 350 and 450 pM in Dex-treated fibroblasts, MCF-7Ca, and JEG-3 cells, respectively). Competitively, but reversibly binds to the heme iron of aromatase. Does not affect the synthesis of adrenal mineralocorticoid or glucocorticoids. Reported to be highly effective as an anti-estrogenic and anti-proliferative agent in estrogen-rich tumors. Also delays the fusing of the growth plates in adolescents and enhances the effectiveness of growth hormone. Shown to synergistically induce apoptosis and cause tumor regression when combined with IGF-1R inhibitors.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Hou, X., et al. 2011. Cancer Res.71, 7597.
Lisztwan, J., et al. 2008. Breast Cancer Res.10, R56.
Miller, W.R., et al. 2002. Cancer Invest.20 (Suppl 2), 15.
Long, B.J., et al. 1998. J. Steroid Biochem. Molec. Biol.67, 293.
Lisztwan, J., et al. 2008. Breast Cancer Res.10, R56.
Miller, W.R., et al. 2002. Cancer Invest.20 (Suppl 2), 15.
Long, B.J., et al. 1998. J. Steroid Biochem. Molec. Biol.67, 293.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Warning
hcodes
Hazard Classifications
Repr. 2 - STOT RE 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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